Process for the preparation of 2-halomethyl-penems and their use for the preparation of antibacterial penems
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United States of America Patent
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Nov 28, 2000
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N/A
app pub date -
Aug 6, 1998
filing date -
Feb 27, 1996
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Expired
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Abstract
Process for the preparation of 2-halomethyl-penems (I) comprising (a) reacting an acetoxy-(protected hydroxyethyl)-2-azetidinone (III) with a 2-halothioacetic acid to form a 3-haloacetylthioazetidinone (V), (b) reacting (V) with oxalyl chloride to give an intermediate (VII), acylated on the beta-lactamic nitrogen, and (c) cyclizing (VII) in the presence of an organic phosphate or phosphonite to produce the corresponding 2-halomethyl-penem (I).
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